The efficacy and safety of toremifene-ifosfamide as a first-line chemotherapy in non-small cell lung cancer were assessed. Sixteen patients were treated with oral toremifene (420 mg on days 1-4 and 240 mg on day 5) followed by ifosfamide infusion 5 g/m2 on day 5 every 3 weeks 1-6 times. Toremifene at the doses used did not enhance the effect or toxicity of ifosfamide in previously untreated non-small cell lung cancer patients.